JPH07277941A - External preparation for skin - Google Patents

Abstract

PURPOSE:To obtain a melanism inhibitor and a cosmetic having excellent inhibitory action on melanism and high safety, containing an extract of bark of Benzoin umbellatum of the family Lauraceae. CONSTITUTION:This external preparation for skin contains 0.01-10wt.% of bark of Benzoin umbellatum of lauraceous plant as it is, powder obtained by drying and finely grinding the bark of Benzoin umbellatum, an extract obtained by extracting bark of Benzoin umbellatum with a polar solvent and removing the solvent or a fraction obtained by fractionating the extract by column chromatography or separating extraction as an active ingredient. The active ingredient is properly mixed with various arbitrary components into an external preparation for skin and a cosmetic and can be prepared into a lotion, a cream, an ointment, a milky lotion, pack, etc.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a melanin production inhibitor and cosmetics containing the same.

[0002]

2. Description of the Related Art It has been a desire of many women to have white and beautiful skin. Even the white skin of a baby gradually loses its beauty due to pigmentation over time as it ages or under the influence of ultraviolet rays. Such pigmentation is caused by the change of tyrosine to dopa and dopa to dopaquinone by tyrosinase, an enzyme biosynthesized in pigment cells, and melanin is produced via intermediates such as 5,6-dihydroxyindole. Has been done.

From such a viewpoint, as a substance that suppresses pigmentation, a sulfur-containing compound such as glutathione or a hydroquinone derivative, which has an activity of inhibiting tyrosinase activity, is
In addition, hydrogen peroxide solution, ascorbic acid and its derivatives that bleach the produced melanin have been developed. However, these have problems such as decomposition, coloring and generation of malodor on the stability and are irreversible. There were many safety problems such as vitiligo formation and rash. Therefore, it is no exaggeration to say that a melanin production inhibitor that can withstand actual use has not yet been developed.

[0004] On the other hand, it was not known that the bark of the camphor tree Chromophyceae contains a substance having an action of suppressing melanin production.

[0005]

SUMMARY OF THE INVENTION The present invention has been made in view of such circumstances, and therefore provides a melanin production inhibitor excellent in safety and suppression of melanin production, and a cosmetic containing the same. This is an issue.

[0006]

[Means for Solving the Problems] From the above viewpoints, the present inventors collect crude drugs that have been used for many years and are considered to be excellent in safety, and conduct screening using melanin production inhibitory action as an index. Again, the inventors have found that the bark of Chromophyceae, a plant of the Lauraceae family, contains a substance having a remarkable melanin production inhibitory effect, and completed the invention.

[0007] That is, the present invention relates to a melanogenesis inhibitor comprising an extract of bark of a camphoraceae plant.

The present invention also relates to an external preparation for skin containing a melanin production inhibitor consisting of an extract of bark of a Lauraceae plant.

The present invention will be described in detail below. It is known that Chromodis which is a camphoraceae plant used as a melanin production inhibitor in the present invention contains balm oil having an antibacterial action and a refreshing sensation in its leaves and stems, but has a melanin production inhibiting action. It is neither known to contain the substance nor how to use it for bark.

The bark extract of Chromophyceae, which is a camphoraceae plant of the present invention, means the bark of these Chromophyceae as it is,
Alternatively, it refers to a product obtained by drying and finely pulverizing, an extract obtained by extracting the bark of Chromodis with a polar solvent and removing the solvent, and a fraction obtained by fractionating the extract by column chromatography or liquid separation extraction.

This is a method for obtaining an extract from the bark of Chromody serrata.
Prior to the extraction operation, the bark of Chromodis may be pre-treated by being dried or crushed. these,
Add 1 to 100 times the amount of solvent to the bark or pretreated bark, and soak for several hours if heated, or for several days if at room temperature,
After removing the insoluble matter by filtration or the like, the solvent may be removed by drying under reduced pressure. The solvent used is preferably highly polar, and examples thereof include one or more selected from water, methanol, ethanol, propanol, butanol, acetone, diethyl ether, chloroform, methylene chloride, dichloroethane and the like.

The extract thus obtained may be blended as it is into an external preparation for the skin, or may be blended after further fractionation and purification by column chromatography or liquid separation extraction. Specific examples of fractional purification include silica gel column chromatography using a methanol diethyl ether solution or chloroform solution as an elution solvent, ODS column chromatography using a methanol aqueous solution or an acetonitrile aqueous solution as an elution solvent, butanol-water, diethyl ether. -Liquid-liquid extraction of water, ethyl acetate-water, hexane-water and the like.

The extract thus obtained, together with various optional components, can be formulated into an external preparation for skin according to a conventional method. The dosage form is not particularly limited as long as it is a conventional one such as lotion, cream, ointment, emulsion or pack.
Further, as an optional component, a polyhydric alcohol, a moisturizer, a thickener, a hydrocarbon, an ester, an alcohol, a higher fatty acid, a surfactant, a powder component, a coloring agent, a fragrance, an antioxidant, an ultraviolet absorber, an anti-aging agent An inflammatory agent etc. can be illustrated. Further, other melanin production inhibitors such as a sulfur-containing compound, an ascorbic acid derivative and a hydroquinone derivative may be added.

The content of the melanin production inhibitor of the present invention in the external preparation for skin is preferably 0.01 to 10% by weight. This is because if the content is less than 0.01% by weight, the effect of suppressing melanin production cannot be expected, and if it exceeds 10% by weight, the effect is flat and the economy is not achieved. The content of the melanin production inhibitor of the present invention in the external preparation for skin is 0.1 to 10% by weight in which the melanin production inhibitory action is more clear.
If so, it is more preferable.

[0015]

The present invention will be described in more detail with reference to examples, but it goes without saying that the present invention is not limited to these examples.

Example 1 Production Example 1 g of a 50% aqueous methanol solution was added to 1000 g of bark of Chromophyllum bark.
0 l was added, and the mixture was heated and stirred under reflux for 3 hours to obtain 1.8 g of melanin production inhibitor 1 as a pale yellow amorphous substance.

Example 2 Melanin production inhibitory action About the melanin production inhibitor of Example 1, melanoma B
The melanin production inhibitory effect was examined using −16 cells. That is, B-16 cells in the logarithmic growth phase were treated with trypsin to give 10% FB at a concentration of 1.5 × 10 ³ cells / ml.
An S (fetal bovine serum) -containing MEM medium suspension was prepared, and 10 ml of each culture bottle was dispensed. This was cultured for 2 days in a CO ₂ incubator. (37 ° C, 5% C
O ₂ ) Various concentrations of melanin production inhibitors were added to this and the culture was continued for 2 days. In the same manner, 15 ml of medium and a melanin production inhibitor were added in the same manner, and the cells were further cultured for 2 days. 6
The medium was removed on the day, washed with PBS (phosphate buffered saline), treated with trypsin, detached from the cells, collected by centrifugation, and visually observed for cytotoxicity and melanin production inhibitory action. It was judged. The criteria for cytotoxicity are
+: Cytotoxic, ±: difficult to determine cytotoxicity, −: no cytotoxicity. The criteria for the melanin production inhibitory action were +: melanin production inhibitory action, ±: melanin production inhibitory action was slightly observed, and-: melanin production inhibitory action was not. The results are shown in Table 1. It can be seen that any of the melanin production inhibitors of the present invention can suppress melanin production even at low concentrations.

[0018]

[Table 1]

Example 3 Safety (Local Toxicity) In order to know the safety of the melanin production inhibitor of the present invention, local toxicity by transdermal administration using Hartley white guinea pig (male, 350 g) was examined. . That is, 0.05% of a 1% ethanol solution of the melanin production inhibitor 1 was applied to a 2 cm square area prepared by shaving the back of a guinea pig.
It was administered once daily for 5 days and the skin reaction was evaluated on the 6th day based on the Japanese patch test standard (Japan Dermatological Association). That is, −: no reaction, ±: false positive reaction, +: positive reaction, ++: reaction accompanied by edema. The results show that all the samples were non-reactive (-), indicating that the melanin production inhibitor of the present invention is highly safe.

Example 4 Formulation Example (Lotion) A lotion was prepared according to the following formulation. That is, the following ingredients were weighed, heated and dissolved at 80 ° C., and cooled to obtain a lotion.
In the following, the numerical values of the prescription indicate parts by weight. Propylene glycol 5.5 Ethanol 10 Methylparaben 0.2 Sodium chloride 0.3 Citric acid 0.1 Sodium acetate 0.1 Perfume 0.1 Polyoxyethylene (50) hydrogenated castor oil 0.5 Water 83.1 Example 1 Melanin production inhibitor 1 0.1

Example 5 Formulation Example (Lotion) Lotion was prepared according to the following formulation. That is, the following ingredients were weighed, heated and dissolved at 80 ° C., and cooled to obtain a lotion. Propylene glycol 5.5 Ethanol 10 Methylparaben 0.2 Sodium chloride 0.3 Citric acid 0.1 Sodium acetate 0.1 Perfume 0.1 Polyoxyethylene (50) hydrogenated castor oil 0.5 Water 82.2 Example 1 Melanin production inhibitor 1 1

Example 6 Formulation Example (Lotion) Lotion was prepared according to the following formulation. That is, the following ingredients were weighed, heated and dissolved at 80 ° C., and cooled to obtain a lotion. Propylene glycol 5.5 Ethanol 10 Methylparaben 0.2 Sodium chloride 0.3 Citric acid 0.1 Sodium acetate 0.1 Perfume 0.1 Polyoxyethylene (50) hydrogenated castor oil 0.5 Water 73.2 of Example 1 Melanin production inhibitor 1 10

Example 7 Formulation Example (Lotion) Lotion was prepared according to the following formulation. That is, the following ingredients were weighed, heated and dissolved at 80 ° C., and cooled to obtain a lotion. Propylene glycol 5.5 Ethanol 10 Methylparaben 0.2 Sodium chloride 0.3 Citric acid 0.1 Sodium acetate 0.1 Perfume 0.1 Polyoxyethylene (50) hydrogenated castor oil 0.5 Water 83.19 of Example 1 Melanin production inhibitor 1 0.01

Example 10 Formulation Example (Cream) A cream was prepared according to the following formulation. That is, A, B
Were weighed and melted by heating at 80 ° C., and B was gradually added to A while stirring to emulsify. This was cooled with stirring to obtain a cream. (A) Cetanol 1 Synthetic Geyrow 2.5 Beeswax 2.5 Stearic Acid 1 Vaseline 3 Squalane 14 Olive Oil 6 γ-Tocopherol 0.1 Perfume 0.1 Butylparaben 0.1 Glyceryl Monostearate 2.5 Polyoxyethylene (25 ) Stearate 2.5 (B) Caustic potassium 0.02 Melanin production inhibitor 1 of Example 1 0.03 Water 56.4 Propylene glycol 8 Methylparaben 0.25

Example 11 Formulation Example (Cream) A cream was prepared according to the following formulation. That is, A, B
Were weighed and melted by heating at 80 ° C., and B was gradually added to A while stirring to emulsify. This was cooled with stirring to obtain a cream. (A) Cetanol 1 Synthetic Geyrow 2.5 Beeswax 2.5 Stearic Acid 1 Vaseline 3 Squalane 14 Olive Oil 6 γ-Tocopherol 0.1 Perfume 0.1 Butylparaben 0.1 Glyceryl Monostearate 2.5 Polyoxyethylene (25 ) Stearate 2.5 (B) Caustic potassium 0.02 Melanin production inhibitor 1 of Example 1 0.01 Water 56.42 Propylene glycol 8 Methylparaben 0.25

Example 12 Formulation Example (Cream) A cream was prepared according to the following formulation. That is, A, B
Were weighed and melted by heating at 80 ° C., and B was gradually added to A while stirring to emulsify. This was cooled with stirring to obtain a cream. (A) Cetanol 1 Synthetic Geyrow 2.5 Beeswax 2.5 Stearic Acid 1 Vaseline 3 Squalane 14 Olive Oil 6 γ-Tocopherol 0.1 Perfume 0.1 Butylparaben 0.1 Glyceryl Monostearate 2.5 Polyoxyethylene (25 ) Stearate 2.5 (B) Caustic potassium 0.02 Melanin production inhibitor 1 of Example 1 0.3 Water 56.13 Propylene glycol 8 Methylparaben 0.25

Example 13 Formulation (Cream) A cream was prepared according to the following formulation. That is, A, B
Were weighed and melted by heating at 80 ° C., and B was gradually added to A while stirring to emulsify. This was cooled with stirring to obtain a cream. (A) Cetanol 1 Synthetic Geyrow 2.5 Beeswax 2.5 Stearic Acid 1 Vaseline 3 Squalane 14 Olive Oil 6 γ-Tocopherol 0.1 Perfume 0.1 Butylparaben 0.1 Glyceryl Monostearate 2.5 Polyoxyethylene (25 ) Stearate 2.5 (B) Caustic potassium 0.02 Melanin production inhibitor 1 of Example 1 0.01 Water 56.42 Propylene glycol 8 Methylparaben 0.25

Example 14 Formulation Example (Foundation) A foundation was prepared according to the following formulation. That is, after kneading A, adding B and further kneading, heating to 80 ° C. and dispersing C, gradually adding and dissolving D heated to 80 ° C. to emulsify, stir and cool to obtain a foundation. (A) Propylene glycol 5 Malbitol 10 Methylparaben 0.3 Diglycerin triisostearate 4 (B) Liquid paraffin 5 Butylparaben 0.1 (C) Titanium oxide 9 Yellow iron oxide 1.7 Bengala 1.2 Talc 8.1 (D) Water 55 Melanin production inhibitor 1 of Example 1 0.6

[0029]

EFFECT OF THE INVENTION The melanin production inhibitor of the present invention is very useful because it is highly safe and has a high melanin production inhibitory action. Therefore, an external preparation for skin containing the same is highly safe and has an excellent melanin production inhibitory action, which is very useful.

 ─────────────────────────────────────────────────── ─── Continuation of the front page (72) Inventor Akiyoshi Matsubara 27 Takashimadai, Kanagawa-ku, Kanagawa-ku, Kanagawa Prefecture 1 Yokohama Research Laboratory, Pola Chemical Industry Co., Ltd. (72) Inventor Takeru 27 Takashimadai, Kanagawa-ku, Yokohama-shi, Kanagawa 1 Polar Chemical Industry Co., Ltd. Yokohama Research Laboratory (72) Inventor Satoshi Ohata 27 Takashimadai, Kanagawa-ku, Kanagawa-shi, Kanagawa Prefecture 1 Polar Chemical Industry Co., Ltd. Yokohama Research Laboratory (72) Inventor Hogo Hogo Takashimadai, Kanagawa-ku, Yokohama, Kanagawa Prefecture 27-1 Polar Chemical Industry Co., Ltd. Yokohama Laboratory (72) Inventor Yoshiyuki Miyata Takashimadai, Kanagawa-ku, Yokohama, Kanagawa Prefecture 27-1 Polar Chemical Industry Co., Ltd. Yokohama Laboratory (72) Inventor Yutaka Sashida Tokyo 3-20-7 Nanyodai, Hachioji City (72) Inventor Yoshihiro Maki 6-20-21 Hirayama, Hino City, Tokyo Heights Hatta No 1-103

Claims (3)

[Claims] 1. A melanin production inhibitor comprising an extract of Chromophyceae bark of the Lauraceae family. 2. A cosmetic containing the melanin production inhibitor according to claim 1. 3. The cosmetic according to claim 2, wherein the content of the melanin production inhibitor according to claim 1 is 0.01 to 10% by weight.